BP1.3656B
BP1.3656B is a selective, orally active, blood-brain barrier-permeable histamine H3 receptor (histamine H3 receptor) inverse agonist/antagonist, with a KB value of 0.08 nM for antagonizing agonist-induced activity and an IC50 value of 0.38 nM for directly inhibiting the basal activity of the receptor. BP1.3656B reduces alcohol consumption, alcohol-seeking behavior, alcohol self-administration, motivation to drink, alcohol relapse, alcohol-induced hyperlocomotion, and binge alcohol intake. BP1.3656B is applicable for the research of alcohol use disorder.
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- No. CAS: 914302-78-6
- Fòrmula: C20H28Cl2N2O2
- Peso molecular:399.35
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
H3 receptor 0.38 nM (IC50) |
In Vivo
BP1.3656B (0.03-0.1 mg/kg; i.p.; single administration) dose-dependently increases extracellular acetylcholine levels in the hippocampus of male Wistar rats[1].
BP1.3656B (0.005-0.3 mg/kg; single administration) reduces alcohol-induced motor hyperactivity in female DBA/2J mice[1].
BP1.3656B (0.3 mg/kg; i.p.; once daily for 4 consecutive days) reduces alcohol-induced locomotor sensitization in female DBA/2J mice by 31%-44% over the 4-day treatment course[1].
BP1.3656B (0.3 mg/kg; i.p.; single administration) reduces alcohol intake by 25% in male mice in the dark drinking model, normalizes anxiety-like behaviors in mice during alcohol withdrawal, and decreases voluntary alcohol intake in non-addicted and alcohol-dependent male rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/2J (female)[1]
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Dosage:0.005 mg/kg; 0.03 mg/kg; 0.3 mg/kg
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Administration:i.p.; single dose
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Result:Reduced alcohol-induced locomotor activity by 37%.
Reduced alcohol-induced locomotor activity by 39%.
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Animal Model:DBA/2J (female)[1]
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Dosage:0.3 mg/kg
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Administration:i.p.; daily; 4 consecutive days
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Result:Reduced alcohol-induced locomotor sensitization by 31% on day 1, 44% on day 2, 25% on day 3, and 40% on day 4.
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Animal Model:C57BL/6J (male)[1]
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Dosage:0.3 mg/kg
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Administration:i.p.; singe dose
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Result:Reduced 2-hour binge alcohol intake by 25%.
Increased time spent in the open arms of the elevated plus maze
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Animal Model:Long Evans (male; non-dependent)[1]
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Dosage:0.3 mg/kg
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Administration:i.p.; single dose
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Result:Reduced active lever presses by 70%, alcohol consumption by 73%, and motivation (breakpoint) by 43% compared to placebo.
Reduced alcohol relapse by 44% on the first day post-extinction, with effects maintained across relapse sessions.
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Animal Model:Long Evans (male; alcohol-dependent)[1]
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Dosage:0.3 mg/kg
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Administration:i.p.; single dose
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Result:Reduced active lever presses by 46%, alcohol consumption by 55%, and motivation (breakpoint) by 44% compared to placebo.
Completely blocked alcohol relapse on the first day post-extinction, with effects maintained across relapse sessions.
Chemical Information
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No. CAS 914302-78-6
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Peso molecular 399.35
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Fòrmula C20H28Cl2N2O2
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SMILES
C[C@H]1CCCN(C1)CCCOC2=CC=C(C=C2)C3=CC=[N+](C=C3)[O-].Cl.Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BP1.3656B Related Classifications
HY-181960 Related Classifications
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